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The present study is aimed towards preparation and characterization of gastroretentive floating m... more The present study is aimed towards preparation and characterization of gastroretentive floating multiparticulate oral drug delivery system of diltiazem hydrochloride, which can provide sustained release delivery of the drug. These gastroretentive floating microspheres release the drug in the stomach and upper gastrointestinal tract and thereby improve the bioavailability. In the present study, six formulations of diltiazem hydrochloride were prepared as gastroretentive floating microspheres by solvent diffusion technique using polymers such as ethyl cellulose, polyvinyl pyrrolidone K-90 and poly vinyl alcohol in different ratios. The prepared floating microspheres were evaluated for different physicochemical tests such as particle size, percent drug entrapment, drug content uniformity, SEM, buoyancy test, and in vitro drug release studies. The results of all the physicochemical tests of all formulations were found to be satisfactory. In vitro floatability studies revealed that most of the microspheres (53.21% to 96.12%) were floatable. The in vitro drug release was found to be in the range of 40.36 to 94.11 % at the end of 6 hours. It is concluded that these floating microspheres can be selected for the development of gastroretentive drug delivery system of diltiazem hydrochloride for potential therapeutic uses.
The aim of present research work was formulation, evaluation and determination of Sun protection ... more The aim of present research work was formulation, evaluation and determination of Sun protection factor of polyhebal sunscreen cream containing oil of Daucus carrota, Simondsia chinensis,Triticum astevum,Olea europaea. On chronic exposure to sun light it causes dilation of blood vessel results in erythema,oedema,suntan, prematuared skin ageing and may increase the risk of skin cancer. Herbal phytoconstituent sunscreen agents either reflect or absorbed UV radiation before reaching to the skin. In this study sun protection factor of formulation was determined by in vitro method spectrophotometrically, two formulations F1 and F2 were prepared by using different concentration of above four herbal oil .they were evaluated for stability,irritation, consistency, homogeneity and pH. Results showed that both F1 and F2 has good stability, homogenicity, good consistency, no irritation occurred and no evidence of phase separation. When compared with marketed formulation it showed good sunscreen activity specially F1 formulation INTRODUCTION The skin is one of the largest organs in the body in surface area and weight [1].Sun rays adversely affect the skin, harmful effects of solar radiation on the skin are premature aging or cutaneous cancer ,basal cell carcinoma, sunburns, malignant melanomas [2]. Solar light consists of different radiations range are UVA in the 320-400, UVB-290-320 and UVC-100-290 nm range respectively. Since long time of period cosmetics products are apply on the body for the purpose of nourishing, to reduce hyper pigmentation and skin wrinkling, cleansing, beautifying, protection or altering appearance and enhancing the beauty. The herbal phytoconstituents or herbal extracts act on this particular area and produce antioxidant effect, relieving erythema, healing, softening, rejuvenating and sunscreen effect. The photoprotective phytoconstituents such as silymarin, geinstein, curcumin, resveratrol, tea polyphenols, , quercetin,flavonoids,glycerrhinitic acid and ascorbic acid which are used for the development of herbal cosmetic formulation.
The aim of the present work was to design controlled release matrix tablets of Cephalexin by inco... more The aim of the present work was to design controlled release matrix tablets of Cephalexin by incorporating the drug in a matrix made up of using combination of hydrophilic and hydrophobic polymers, which prolong drug release to provide patient convenience. Hydrophilic and hydrophobic polymers such as hydroxypropyl methylcellulose of different grades and ethyl cellulose respectively, as carriers in various concentrations were used to study their release pattern and release mechanism of the drug from matrix tablets upto 12 hours. Matrix tablets were formulated with 1:1, 1:2, 1:3 and 1:4 hydrophobic to hydrophilic polymer ratio. F1 to F4 formulation were prepared with ethylcellulose and HPMC K4M in 1:1, 1:2, 1:3, 1:4, 2:1, 2:2, 2:3, 2:4, 3:1, 3:2, 3:3 and 3:4. Similarly, F5 to F8 were prepared with ethylcellulose and HPMC K15M and, and F9 to F12 were prepared with ethylcellulose and HPMC K100M and by dry granulation technique. Designed matrix tablets were evaluated for various pre-compression and post-compression parameters. F4 is the best formulation, showed 100.34% release at the end of 12 h as it showed good similarity factor as compared with theoretical release rate profile. Drug released pattern followed zero order with non-Fickian diffusion method. INTRODUCTION In developing countries, infectious diseases are very often. The infectious diseases are precipitated by both gram positive and gram negative bacteria hence, the treatment is necessary with broad spectrum of activity. All cephalosporin posses a wide range of bactericidal activity. Cephalexin is an orally active first generation cephalosporin, which has high activity against gram-positive bacteria, these act by inhibiting bacterial cell wall synthesis [1][2]. Controlled release dosage forms have number of advantages over conventional dosage forms, such as improved patience compliance due to decrease in dosing frequencies, reduction in fluctuation in steady-state levels and therefore better control of disease, maximum utilization of drug enabling reduction in total amount of dose administered[3][4].In the present work, an attempt has been made to design, formulate and evaluate in-vitro release of cephalexin matrix tablets. As the effect
The objective of present investigation is to offer controlled release of aceclofenac in the intes... more The objective of present investigation is to offer controlled release of aceclofenac in the intestinal zone from a novel multipartculate pulsatile system filled with mixed blend polymer microcapsules to achieve the chronotherapy of rheumatoid arthritis. Seven batches of microbeads with varying concentration of sodium alginate (2-5 %w/v) were prepared by ionotropic-gelation method using CaCl 2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% w/v Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596.45±1.04 to 860.10±1.14 micron and %DEE in the range of 65.43-84.5%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27.17 and 25.4% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol. INTRODUCTION Chronopharmacotherapy for rheumatoid arthritis has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Chronotherapeutics refers to a treatment method in which in-vivo drug availability is timed to match rhythms of disease in order to optimize therapeutic outcomes and minimize side effects. The half-life of anti-inflammatory drug aceclofenac is around 4 hours, protein binding of 99.7% and the usual dose is 100 mg. A pulsatile drug delivery system that can be administered at night (before sleep) but that release drug in early morning would be a promising chronopharmaceutics system. Drug pharmacokinetics too shows circadian variation for various anti-inflammatory drugs which have
Context: Two 1-day fentanyl transdermal formulations (FTFs)Fentos ® Tape of gum base and OneDuro... more Context: Two 1-day fentanyl transdermal formulations (FTFs)Fentos ® Tape of gum base and OneDuro ® Patch of acrylate baseare marketed in Japan. Objective: To examine the effects of skin surface temperature and abrasion, as well as adhesive bases on the hairless rat skin permeability of fentanyl. Materials and Methods: Permeability was examined in vitro for 24 hours under the following study conditions: skin surface temperatures (32, 37, and 40C) and skin abrasion (intact and abraded). The flux (Js) rates of fentanyl were calculated. Furthermore, Arrhenius plots were constructed to examine the correlation between skin permeability and skin surface temperature. Results: We compared the Js values of these FTFs in the intact and abraded skin at 32C. Consequently, FTFs showed the significantly higher (P < 0.05) Js values in the abraded skin than in the intact skin. The slope was steeper for Fentos ® Tape than for OneDuro ® Patch. Discussion and Conclusion: The effects of skin surface temperature on skin permeability were greater for Fentos ® Tape than for OneDuro ® Patch. Compared to skin intactness, the influences of skin abrasion on skin permeability of fentanyl were greater for both FTFs. Heed needs to be given to skin conditions when using these FTFs in clinical practice.
The aim of this study was to investigate swelling and erosion behaviors of hydrophilic matrix tab... more The aim of this study was to investigate swelling and erosion behaviors of hydrophilic matrix tablets using ethyl cellulose and its impact on drug release. The matrix tablets were prepared by wet granulation method. Swelling and erosion studies of ethyl cellulose matrix tablets were carried out in 6.8 pH phosphate buffer media. The ethyl cellulose matrix tablets formed a continuous gel layer while in contact with the aqueous medium undergoing a combination of swelling and erosion. Formulation F3 found to be optimized formula as it shows slow drug release, which is must for sustained release formulation. The release data showed a good fit into the power law or the Korsmeyer–Peppas equation indicating the combined effect of diffusion and erosion mechanisms of drug release.
Microspheres constitute an important part of novel drug delivery system by virtue of their small ... more Microspheres constitute an important part of novel drug delivery system by virtue of their small size and efficient carrier capacity. Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers having a particle size ranging from 1-1000 µm. The range of Techniques for the preparation of microspheres offers a Variety of opportunities to control aspects of drug administration and enhance the therapeutic efficacy of a given drug. There are various approaches in delivering a therapeutic substance to the target site in a sustained controlled release fashion. One such approach is using microspheres as carriers for drugs also known as micro particles. It is the reliable means to deliver the drug to the target site with specificity, if modified, and to maintain the desired concentration at the site of interest. Microspheres received much attention not only for prolonged release, but also for targeting of anticancer drugs. The purpose of the review is to compile various types of microspheres used in the formulation of microsphere drug delivery system and its applications.
Migraine is more than just a headache. In fact, it is defined as a recurrent headache disorder th... more Migraine is more than just a headache. In fact, it is defined as a recurrent headache disorder that is associated with nausea and/or vomiting, phonophobia, or photophobia. The aim of the present work was preparing the sublingual tablet which consists of a combination of ergotamine, caffeine and cyclizine for the treatment of Migraine. The Sublingual tablets were prepared by direct compression procedure using different concentration of superdisintegrants and microcrystalline cellulose. Precompression and Postcompression parameters such disintegration time, wetting time, water absorption ratio, in vitro drug release and stability study of optimized formulation were determined. The result obtained revealed that the precompression parameters were in acceptable range of pharmacopoeial specification. The disintegration time of optimized formulation (F3) was upto 30 sec. The in vitro release of the drugs was upto 45 min.
Most viral diseases, with the exception of those caused by human immunodeficiency virus, are self... more Most viral diseases, with the exception of those caused by human immunodeficiency virus, are self-limited illnesses that do not require specific antiviral therapy. The currently available antiviral drugs target 3 main groups of viruses: herpes, hepatitis, and influenza viruses. With the exception of the antisense molecule fomivirsen, all antiherpes drugs inhibit viral replication by serving as competitive substrates for viral DNA polymerase. Drugs for the treatment of influenza inhibit the ion channel M 2 protein or the enzyme neuraminidase. Combination therapy with Interferon-α and ribavirin remains the backbone treatment for chronic hepatitis C; the addition of serine protease inhibitors improves the treatment outcome of patients infected with hepatitis C virus genotype 1. Chronic hepatitis B can be treated with interferon or a combination of nucleos(t)ide analogues. Notably, almost all the nucleotide analogues for the treatment of chronic hepatitis B possess anti–human immunodeficiency virus properties, and they inhibit replication of hepatitis B virus by serving as competitive substrates for its DNA polymerase. Some antiviral drugs possess multiple potential clinical applications, such as ribavirin for the treatment of chronic hepatitis C and respiratory syncytial virus and cidofovir for the treatment of cytomegalovirus and other DNA viruses. Drug resistance is an emerging threat to the clinical utility of antiviral drugs. The major mechanisms for drug resistance are mutations in the viral DNA polymerase gene or in genes that encode for the viral kinases required for the activation of certain drugs such as acyclovir and ganciclovir. The potential pharmacokinetic interactions between didanosine, an acid-labile antiretroviral agent, and ranitidine, an H2-receptor antagonist, were evaluated by a crossover study of 12 male and/or ranitidine by validated high-performance liquid chromatography-UV assay methods.
In present era, many research and technological advancements are made in the field of oral drug d... more In present era, many research and technological advancements are made in the field of oral drug delivery as it is highly accepted amongst patient. In this research the formulation of Antihyperlipidemic Chewing gum of Simvastatin using Water insoluble Gum base Water soluble other portion containing Drug as well as Excipients like taste masking agent Sorbital which use as a coating agent in this formulation. The Primary and important requirement in the formulation of Simvastatin Chewing gum is the Gum Base ,Which give it Gummy texture for Chewing Action and as a Drug Vehicle .This gum is Isolated from the natural sources like a Sapodilla Monikara tree (Chiku)which fully grow in the Maharashtra region .This gum base have a property as like other gum bases which is present in nature .For the improvement in the stability of that gum base ,which is converted in the dry form by drying and adding filler as talc and emulsifier such lecithin which was freshly collected from egg yolk .By drying this mixture further it convert in a Directly compressible gum Base Powder , Which possess all important flow property which require for Direct Compression. Direct Compression is one of the best method as compare to moulding method in the formulation of Chewing gum .For direct compression in directly compressible gum require other additional excipients like Antiadherant, Anti-Caking Agent, Lubricant, Antioxidant , Flavor ,and Sweetening, Coating Agent (Sorbital). For evaluation of formulated chewing gum all parameter are same as like Tablet except In-vitro drug release performance. For this purpose , the Disintegration Apparatus was modified in such way that it continuously Compress or crush the chewing gum as like our mastication activity in the mouth, resulting in releases of drug in the salivary fluid and absorbance were calculate on U. V. Visible Spectra. In this also study the effect of Stroke & Distance Between jaw which gives the valuable information about Drug release performance in various ages Patient.
Drug delivery via the oral mucous membrane is considered to be a promising alternative to the ora... more Drug delivery via the oral mucous membrane is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired with better patient compliance than orally ingested tablets. In terms of permeability, the sublingual area of the oral cavity (i.e. the floor of the mouth) is more permeable than the buccal (cheek) area, which in turn is more permeable than the palatal (roof of the mouth) area. The portion of drug absorbed through the sublingual blood vessels bypasses the hepatic first‐pass metabolic processes giving acceptable bioavailability. Sublingual technology for patients need enhanced lifecycle management to convenient dosing for geriatric, pediatric and patient with dysphagia. This review highlights the sublingual dosage forms for the treatment of migraine, factors affecting the sublingual absorption, advantages, various in vitro and in vivo evaluation parameters and commercially available sublingual dosage forms. INTRODUCTION Oral administration is a route of administration where a substance is taken through the mouth. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream. Tablet is defined as a compressed solid dosage form containing medicaments with or without excipients. According to the Indian Pharmacopoeia Pharmaceutical tablets are solid, flat or biconvex dishes, unit dosage form, prepared by compressing a drugs or a mixture of drugs, with or without diluents. They vary in shape and differ greatly in size and weight, depending on amount of medicinal substances and the intended mode of administration. It is the most popular dosage form and 70% of the total medicines are dispensed in the form of Tablet. (1) Solid medicaments may be administered orally as powders, pills, cachets, capsules or tablets. These dosage forms contain a quantity of drug which is given as a single unit and they are known collectively as solid unit dosage forms, even in the case of sustained action preparations which, technically, contain the equivalent of several normal doses of drug. (2) Tablet that disintegrates or dissolve rapidly in the patients mouth are convenient for young children, elderly patients, mentally retarded and bedridden patients who used to suffer most probably with the problem of dysphagia and hand tremors. A fast dissolving sublingual tablet when placed in the mouth, rapidly get dispersed or dissolved and swallowed in the form of liquid. When sublingual tablets placed under the tongue, it produces immediate systemic effect by enabling the drug absorbed quickly or directly through mucosal lining of the mouth beneath
Microsponge technology is novel technique generally used for transfer of active drug into the ski... more Microsponge technology is novel technique generally used for transfer of active drug into the skin. It is a controlled release secretion system also helps to reduce systemic exposure and minimize local cutaneous reactions to active drugs. Microsponges used to control delivery of drug at specific predetermined site in body. The Microsponge Delivery System (MDS) is a unique technology for the controlled release of topical agents and consists of macroporous beads, typically 10-25 microns in diameter, loaded with active agent. Microsponges can entrapped various types of drug and incorporated in formulation such as cream, powder, gels and lotions. When applied to the skin; the microsponge releases its active ingredient on a time mode and also in response to other stimuli (rubbing, temperature, pH, etc) also microsponges are taken orally route. Microsponge technology offers entrapment of active drug ingredients and is used in to reduced side effects, improved stability, increased elegance, and enhanced formulation flexibility. The microsponge systems are non-irritating, non-mutagenic, non-allergenic, and non-toxic. Microsponges also inhibit the various problems than other formulation problem such as need of regular dosing, drug reaction; incompatibility with environmental condition also easily stop the treatment and no need of special knowledge. The present review introduces Microsponge technology along with its method of preparation, characterization, advantages and release mechanism of MDS. INTRODUCTION Various systems were developed for systemic drugs under the class of trans-dermal delivery system (TDS) using the skin as portal of entry. Topical drugs while applying having many problems such as ointments, which are often aesthetically unappealing, greasiness, stickiness etc. that often results into lack of patient compliance. Also gels, powders, lotion has low time of contact with skin therefore these vehicles require high concentrations of active agents for effective therapy because of their low efficiency of delivery system no longer drug can be absorb form skin. This problem can be recovered by the microsponges. Microsponges require low drug content but having the longtime of contact with skin. Resulting into no irritation and allergic reactions are observed in some patient. A Microsponge Delivery System (MDS) is patented, highly cross-linked, porous, polymeric microspheres that can entrap wide range of actives and then release them with desired rate[1].This system is useful for the improvement of performance of topically applied drugs. It is a unique technology for the controlled release of topical agents and consists of microporous beads, typically 10-25 microns in diameter, loaded with active agent. Their high degree of cross-linking results in particles that are insoluble, inert and of sufficient strength to stand up to the high shear commonly used in manufacturing of creams, gels, lotions, and powders. Their characteristic feature is the capacity to adsorb or " load " a high degree of active materials into the particle and on to its surface[2].Microsponges should be
Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused by groups ... more Periodontitis is an inflammatory disease of the supporting tissues of the teeth caused by groups of specific microorganisms. Local delivery of antibiotics has been investigated for the possibility of overcoming the limitations of conventional therapy. The goal of this research work is to prepare nanoparticles of minocycline hydrochloride,then these tiny particles are formulated into in situ gels as a local drug delivery system within the periodontal pockets for the effective treatment of periodontitis. FTIR studies indicated that there was no chemical interaction between drug and polymer and stability of the drug. Nanoparticles containing Minocycline hydrochloride were developed by using eudragit RL 100 as polymer andthey were evaluated for drug content, particle size analysis and stability studies. The average particle size of minocycline nanoparticles were within the range. On the other hand optimized formulations of in situ gels containing nanoparticles and pure drug were prepared by using gellan gum (0.6 % w/v) and comparative in vitro diffusion study have done for these in situ gel formulations. No appreciable difference was observed in the extent of degradation of product during 60 days in which nanoparticles were stored at 40°C/ 75% RH.
Nanoemulsions are transparent or translucent dispersions,having the droplet size less than 100 nm... more Nanoemulsions are transparent or translucent dispersions,having the droplet size less than 100 nm with ultra low interfacial tension,large o/w interfacial areas and long term physical stability Recently,much attention has been paid to the application of nanoemulsion as drug delivery systems, since nanoemulsions are thermodynamically stable and are formed spontaneously by simple mixing of various components.An attempt to combine the two phases require energy input to establish water – oil contacts that would replace the water-water and oil-oil contacts.The interfacial tension between bulk oil and water can be as high as 30-50 dynes/cm.To overcome this, surfactants can be used because they contain water loving (hydrophilic) and oil loving (lipophilic) moietie and they tend to adsorb at the water-oil interface.If enough surfactant molecules are present, they align and create an interface between the water and the oil by decresing the interfacial tension.
The primary aim of the study has been to investigate the effect of nano layer distribution in lat... more The primary aim of the study has been to investigate the effect of nano layer distribution in latex matrix, on the mechanical properties, of the latex-nano particle composites. The nano particles selected are organically modified nano clay. It was observed that the key for nano composite technology is the exfoliation of the nano particles into their individual platelets. In this study nano clay is used as filler and is separately incorporated into the latex matrix and the corresponding nano composites are prepared by co-vulcanization method. The mechanical properties are measured and compared with the corresponding macroscopic latex-clay composites. The study reveals that there is a remarkable increase in the properties when nano clay is used as filler in the latex matrix due to the improved latex-nano particle interaction and better homogeneity in the distribution of nano particles in the latex matrix. The effects of nanolayer reinforcement are manifested in terms of reduced swelling by solvents and higher modulus values in the latex-nano particle composites. Tunneling electron microscopic studies (TEM) are conducted to evaluate the extent filler-latex interaction.
Gastro retentive drug delivery is an approach to prolong gastric residence time, thereby targetin... more Gastro retentive drug delivery is an approach to prolong gastric residence time, thereby targeting site-specific drug release in the upper gastrointestinal tract (GIT) for local or systemic effects. The objective of this work is to develop GFDDS of amlodipine, employing swellable polymer hydroxypropylmethylcellulose (HPMC) of different viscosity grades (K100M and K4M) and sodium bicarbonate as gas generating agent, and to evaluate the effect of polymer concentration on amlodipine release from the prepared GFDDS. Twevel formulations of floating tablets of amlodipine besylate using the polymer of different grades namely Hydroxy Propyl Methyl Cellulose K100M (HPMC K 100 M), and Hydroxy Propyl Methyl Cellulose K4 M (HPMC K 4M) in different concentrations were prepared separately by direct compression method. The formulations were evaluated for various physical parameters, buoyancy studies, dissolution parameters and drug released mechanisms. Among all the formulations, formulation F12 containing drug prepared with HPMC K4M and carbopol, showed promising result releasing 98.8% of drug in 12 hrs with a floating lag time of 56 seconds and duration of floating time is 12hrs. INTRODUCTION Floating drug delivery systems were first described by Davis in 1968 [1]. It is possible to prolong the gastric residence time of drugs using these systems. Several techniques are used to design gastro retentive dosage forms. These include, floating drug delivery systems (FDDS), high density DDS, muco-adhesive systems, swelling and expanding DDS, modified shape systems, and other delayed gastric devices. Floating drug delivery systems, also called as hydrodynamically balanced system, is an effective technology to prolong the gastric residence time in order to improve the bioavailability of the drug. This technology is suitable for drugs with an absorption window in the stomach or in the upper part of small intestine, drugs acting locally in the stomach and for the drugs that are poorly soluble or unstable in the intestinal fluid. Effervescent floating drug delivery systems generate gas (CO2), thus reduce the density of the system and remain buoyant in the stomach for a prolonged period of time and released the drug slowly at a desired rate. Amlodipine is long acting calcium channel blocker and used in the treatment of hypertension, and chronic stable angina. In hypertension or angina, initially 5 mg. one daily and adjusted to maximum dose 10 mg one daily dose of Amlodipine is
Rosuvastatin, a HMG-CoA reductase inhibitor widely used in treatment of Hyper(dys)lipidemia cause... more Rosuvastatin, a HMG-CoA reductase inhibitor widely used in treatment of Hyper(dys)lipidemia causes myotoxicity and hepatotoxicity. These safety issues limit dose of Rosuvastatin, lead to additional monitoring of the patients as well as discontinuation of therapy. To alleviate the adverse effects and to improve efficacy and safety profile, Rosuvastatin was encapsulated in nanoparticulate formulation and compared with marketed reference formulation (Crestor tablets). The nanoparticles (NPs) were prepared using single emulsion diffusion method and optimized for particle size, PDI, zeta potential, encapsulation efficiency. The efficacy and safety of final formulation was evaluated in HFD induced hyperlipidemic albino rats. The results suggested that the NPs have significant improvement of efficacy and reduction of the toxicity in comparison to marketed reference formulation. By encapsulating the Rosuvastatin in the NPs, the 50% dose reduction can be achieved without compromising efficacy.
In recent years, considerable attention has been focused on the development of drug delivery syst... more In recent years, considerable attention has been focused on the development of drug delivery system. There are number of reasons for the intense interest in new system. Recognition of the possibility of repeating successful drugs by applying the concepts and techniques of controlled release parenteral depot formulation drug delivery systems coupled with the increasing expense bringing new drug entities to market has encouraged the development of new drug delivery system. New systems are needed to deliver the novel, genetically engineered pharmaceuticals, i.e. peptides and proteins to their site of action without incurring significant immunogenic or biological inactivation. Treating enzyme deficient disease and cancer therapies can be improved by better targeting. Therapeutics efficacy and safety of drugs, administered by conventional methods, can be improved by more precise spatial and temporal placement within the body. Thereby reducing both size and number of doses. INTRODUCTION Primarily due to the steadily increasing number of biotechnology-derived drugs, parenteral depot formulations and their drug delivery technologies have received much attention in recent years. For many compounds which cannot be administered via the oral route, injectable or implantable depot formulations are presently the only viable option for reducing the frequency of administration, thereby increasing patient convenience and potentially improving compliance. Depot formulations have been developed for a broad range of applications, providing therapeutic effectiveness over periods ranging from one day to several years. A significant patient benefit, which should be the driving force for initiating the development of any depot formulation, not only requires that the dosing frequency can be substantially reduced in comparison with the corresponding standard formulation, but also that dosage form-related risks, such as dose dumping or poor carrier tolerability, are largely avoided. The Parenteral administration route is the most effective and common form of delivery for active drug substances with metabolic bio-availabilities drug for which the bio-availability in limited by high first pass metabolism effect of other physicochemical limitation and for drugs with a narrow therapeutic index. For this reason, whatever drug delivery technology that can reduce the total number of injection throughout the drug therapy period will be truly advantageous not only in terms of compliance, but also for potential to improve the quality of the therapy. Such reduction in frequency of drug dosing is achieved, in practice, by the use of specific formulation technologies that guarantee that the release of the active drug substance happens in a slow and predictable manner[1] .
The objective of the present study was to prepare and evaluate sustain release matrix tablets of ... more The objective of the present study was to prepare and evaluate sustain release matrix tablets of Losartan potassium using natural polymers. Tablets were prepared by wet granulation method using different drug: polymer concentrations. Natural gums like karaya gum, Tara gum and locust bean gum were used as release retardant polymers. Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) study revealed no chemical interaction between drug and polymers used. Pre compression and post compression parameters complied with the Indian Pharmacopoeial limit for the tablets. The effect of diluents type, polymer type used and its increase in concentration on the drug release was studied in this work. In-vitro dissolution studies were carried out in 0.1 N HCl for 2h and pH 6.8 buffer for next 10 h. In all the formulations as the concentration of the polymer was increased, drug release was retarded accordingly. The mechanism of drug release for all the formulations was found to be by anomalous transport i.e. by swelling coupled with diffusion from the polymer. Most of the formulations followed zero order kinetics with n value > 0.5. Formulation FV was selected as the best formulation with about 95.11% drug release within 12 h.
Rosuvastatin calcium is a low bioavailable drug used for the management of hyperlipidemia. Buccoa... more Rosuvastatin calcium is a low bioavailable drug used for the management of hyperlipidemia. Buccoadhesive tablets of rosuvastatin calcium were prepared by direct compression method using HPMC K4M, HPMC K15M and carbopol 974P as mucoadhesive polymers and evaluated for in vitro drug release, in vitro bioadhesion, ex vivo residence time, swelling index, surface pH and ex vivo drug permeation. Fifteen formulations were developed with varying concentrations of polymers. Formulations from F1 to F5 were composed of HPMC K4M, F5 to F10 using HPMC K15M and F11 to F15 using carbopol 974. The ratio of drug and polymer were varied from 1:1 to 1:5 in F1 to F10 and 1:0.25 to 1:1.50 in F11 to F15. Formulation F3 showed maximum release of the drug (97.83 ± 0.41%), and from the same formulation maximum drug has permeated (73.14 ± 0.13%) through porcine buccal membrane with a flux of 8.35 ± 0.291µg h-1 cm-2 , permeation coefficient of 1.34 ± 0.05 cmh-1 and maximum bioadhesive force of 24.64±0.246 respectively. FTIR results showed no evidence of interaction between the drug and polymers. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.
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